61 results about "Cefmenoxime Hydrochloride" patented technology

The invention relates to a cefmenoxime hydrochloride composition powder injection, which comprises the following components: 100-150 parts of cefmenoxime hydrochloride, 30-35 parts of natrium carbonicum calcinatum, preferably 125 parts of cefmenoxime hydrochloride and 33 parts of natrium carbonicum calcinatum. The grain size of the cefmenoxime hydrochloride is 400-600 meshes, which is preferably 500 meshes. The manufacturing method of the cefmenoxime hydrochloride composition powder injection comprises the steps as follows: 100-150 parts of cefmenoxime hydrochloride and 30-35 parts of natrium carbonicum calcinatum are respectively sieved, evenly mixed and pulverized until the grain size of the cefmenoxime hydrochloride is 400-600 meshes and is preferably 500 meshes; the obtained powder is sub-packaged into sterilized vials and is plugged. The cefmenoxime hydrochloride composition powder injection prepared by the invention has the advantages of fine quality, rapid dissolution and good stability after being prepared into solution.

The invention relates to a cefmenoxime hydrochloride compound, which is prepared through acid-base reaction, activated carbon adsorption, separation and purification of prepared chromatography so as to achieve the aim of purification and obtain the high-purity cefmenoxime hydrochloride compound finally. The invention optimizes the product quality, and guarantees safety of clinical medication.

The invention provides a cefmenoxime hydrochloride preparation for injection and a preparation method thereof. The main components of the cefmenoxime hydrochloride preparation are soyabean lecithin for injection, cholesterin and cefmenoxime, and the weight ratio of the soyabean lecithin, the cholesterin and the cefmenoxime is 10-2:4-1:1. The preparation method comprises the following steps: dissolving the soyabean lecithin and the cholesterin with absolute ethyl alcohol, adding buffer solution for complete hydration, and filtering with a microporous filter membrane of 0.8mum twice to obtain a blank liposome, then adding the cefmenoxime and NaHCO3 solution, adding water for injection after being evenly mixed, preserving heat in a water bath, and promptly cooling with cold water to obtain a cefmenoxime liposome preparation. The cefmenoxime hydrochloride preparation can achieve the same curative effect as the conventional cefmenoxime for injection at a low dose of the cefmenoxime and reduces adverse reaction caused by the cefmenoxime, thus causing the products to be safer and more effective.

The invention relates to a cefmenoxime hydrochloride compound used for injection which is a crystal. X-ray powder obtained through Cu-K alpha ray measurement is diffracted at a 2 theta of 6.0 degree, 7.4 degree, 11.0 degree, 12.2 degree, 17.5 degree, 19.8 degree, 21.6 degree, 24.8 degree and 27.7 degree with characteristic peaks shown. The main granularity of the cefmenoxime hydrochloride crystal is 30-45 Mum and the distribution width of the cefmenoxime hydrochloride crystal is 25-75 Mum. Injections prepared through the cefmenoxime hydrochloride compound not only are rapid to dissolve and applicable to clinical application, but also have excellent stability, and are safe and reliable.

The invention relates to a novel preparation method of cefmenoxime hydrochloride, which comprises the steps of taking 7-ATCA.HCl as a starting raw material, performing acylation reaction with AE-active ester to produce 7-(alpha-(2- aminothiazole-4-group)-Z-2-methoxy imino group acetamido)-3-cephem-4-carboxylic acid, and finally reacting with hydrochloric acid to produce the cefmenoxime hydrochloride. The method is simple to operate, has high yield, greatly shortens technology time, and is extremely good for indusial production. The cefmenoxime hydrochloride prepared by the method is stable inquality, and the color grade and the impurity level of the cefmenoxime hydrochloride prepared by the method are better than those of cefmenoxime hydrochloride prepared by other methods.

The invention discloses a method for preparing cefmenoxime hydrochloride, which comprises the following steps: uniformly mixing 7-ACT hydrochloride shown in a formula II and AE active ester shown in a formula III under the condition that methylene dichloride and a solvent exist for condensation reaction and obtaining the cefmenoxime hydrochloride shown in a formula I after reaction. The method has the benefits that the cefmenoxime hydrochloride can be synthesized in one step, the cefmenoxime hydrochloride is not required to be separated, a reversely-dropping crystallization method is adopted, the synthetic line is short, the cost is low, the reaction conditions are wild, and the production is convenient; and the cefmenoxime hydrochloride product is high in yield and purity and low in color grade and has an important application value.

The invention discloses a method for synthesizing cefmenoxime hydrochloride. The method comprises the following steps: dissolving 7-ATCA or 7-ATCA hydrochloride and AE-active ester in dichloromethane, and dropwise adding organic alkali at -5-15 DEG C; adding water to extract for multiple times after the reaction is completed, decolorizing the water phase, adding a hydrophilic solvent, and dropwise adding hydrochloric acid at 10-35 DEG C to crystallize and separate cefmenoxime hydrochloride. According to the method for synthesizing cefmenoxime hydrochloride, the condensation system reacts by adopting a single solvent with high conversion rate, and the solvent is convenient to reclaim; the method for synthesizing cefmenoxime hydrochloride is direct crystallization and separation, and adsorption and other separation methods are not needed, so that cefmenoxime hydrochloride has good crystalline form, is easy to separate and dry, simple in synthesizing route and low in cost, and is suitable for industrial production.

The invention provides a cefmenoxime hydrochloride compound entity used for children. The structural formula is as shown in specifications. The cefmenoxime hydrochloride compound entity is prepared through the steps that step1, water is added into a cefmenoxime hydrochloride crude product, sodium carbonate is added, stirring is performed for dissolving, an extracting agent is added, and then the cefmenoxime hydrochloride crude product is transferred into a pressure-resistant container in a filling mode, vibrated in a sealed mode after being defoamed and taken out after being frozen in a temperature control mode; step2, an organic phase is removed, after a solid is melted, active carbon is added, stirring is performed for discoloring, and filtering is performed; step3, pH of filtrate is adjusted to 1.5-2.3 through hydrochloride acid, and then crystal growing, filtering, washing with water and vacuum drying at 40 DEG C are performed to obtain the cefmenoxime hydrochloride compound entity. The cefmenoxime hydrochloride prepared through the method has the advantages of having few impurities, being high in purity and the like compared with a traditional technology.

The invention discloses a new crystal form cefmenoxine hydrochloride compound and a crystallization preparation method thereof. The new crystal form cefmenoxine hydrochloride compound is prepared by adopting the particle process crystal product molecular assembling and morphology optimizing technology. The compound has the advantages of being high in purity and good in fluidity and stability. The invention also discloses a preparation which is prepared from the cefmenoxine hydrochloride compound, namely cefmenoxine hydrochloride for injection.

The invention relates to the field of pharmacy, and especially related to a cefmenoxime hydrochloride compound and a synthesizing method thereof. The cefmenoxime hydrochloride compound has a formula shown below, and is prepared with a method comprising the steps that: (1) a cefoperazone precursor 7-ATCA.HCl and AE active ester are subjected to a condensation reaction under the existence of CH2Cl2and an alkalizing agent; and the obtained product is subjected to extraction, decolorization, press-filtration, neutralization, rejection filtration, and drying, such that cefmenoxime acid CMX-H is prepared; (2) the cefmenoxime acid is completely dissolved by using sodium carbonate; the obtained product is subjected to decolorization, press-filtration, neutralization, decolorization, filtration, crystallization, washing, and drying, such that a cefmenoxime hydrochloride half-finished product is prepared; a jet mill is started; and the material is crushed and is filled in aluminum bottles. According to the invention, cefmenoxime acid is prepared into crystals, such that the product purity is greatly improved, and the product quality is ensured. Also, the method provided by the invention is advantaged in small three-waste volume, simple preparation process, and low cost. Therefore, the method is suitable for the industrialized productions of our nation.

The invention discloses a micro-balloon injection for a pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate, which is characterized by comprising cefmenoxime hydrochloride, anhydrous sodium carbonate, polylactic acid- polyethylene glycol block copolymer, poloxamer 188, glycerol and mannitol. The optimal scheme of the invention is the micro-balloon injection for the pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate, which is characterized by comprising 1 part of cefmenoxime hydrochloride, 0.12-0.18 part of anhydrous sodium carbonate, 1.2-4.5 parts of polylactic acid- polyethylene glycol block copolymer, 0.8-2 part(s) of poloxamer 188, 0.5-1 part of glycerol and 3-6 parts of mannitol. Compared with the prior art, the micro-balloon injection for the pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate prepared by the invention has high stability, the preparation process is simple and is suitable for industrial production, and has high encapsulation efficiency. As anhydrous sodium carbonate is used as a latent solvent, the re-dissolution is good, and has an appropriate slow-release effect.

The invention relates to a method of preparing cefmenoxime E isomers and is applicable to the need of pharmaceutical enterprises. The method comprises the steps: step (1), suspending 3-[[(1-methyl-1H-tetrazole-5-yl) sulfur] methyl]-7-amino-carboxylate hydrochloride dehydrate (7-ATCA.HCl) and trans AE active ester in a mixed system of water and organic solvent, adding alkaline, stirring and reacting to generate the cefmenoxime E isomers, in which the molar rate of the 3-[[(1-methyl-1H-tetrazole-5-yl) sulfur] methyl]-7-amino-carboxylate hydrochloride dehydrate, the trans AE active ester and the alkaline is 1: 1.1-1.3: 2.5-2.8, and the reaction time is 1-3 hours; step (2) after the reaction is finished, passivating, regulating the pH value to be 2.0-3.0, crystallizing, filtering and drying in vacuum. The prepared cefmenoxime E isomers have high purity which is not less than 97%, and can be used as reference substances for quality control of cefmenoxime hydrochloride bulk drug and preparations thereof.

The invention discloses a 1/4 water cefmenoxime hydrochloride compound and a pharmaceutical composition thereof. Cefmenoxime hydrochloride per mole contains 1/4 mole of water. 7 amino cephalosporanicacid (7ACA) is taken as a starting raw material, is firstly reacted with 5-fluorenyl 1 methylol 1H-tetrazolium (MMT) at a C-3 position to form 3-(1-methyl-1-tetrazolium-5H-group) thiomethyl-7-aminocephalosporanic acid (7ACT), is reacted with MAEM in a C-7 position to synthesize cefmenoxime, and then is formed into salt with hydrochloric acid to obtain the 1/4 water cefmenoxime hydrochloride compound. The operation is simple, reactants are easily available, reaction conditions are mild, and the yield is high. The 1/4 water cefmenoxime hydrochloride compound has low moisture absorbing property,low impurity content, good fluidity, good thermodynamic stability and wide application prospect.

The invention belongs to the technical field of medicines, and discloses a method for preparing a cefmenoxine hydrochloride raw material. The method comprises the following steps: enabling 7-ACT as a raw material to react with AE active ester, and adjusting with hydrochloric acid so as to generate a crude product of cefmenoxine hydrochloride; adding L-glutamic acid at normal temperature, heating, adding diethanol amine, cooling, and adding ethyl acetate, thereby obtaining a novel cefmenoxine hydrochloride raw material. By adopting the method disclosed by the invention, the content of macromolecule impurities in cefmenoxine hydrochloride is smaller than 0.1%, and the cefmenoxine hydrochloride raw material can be completely dissolved within 5 seconds.

The invention discloses a cefmenoxime hydrochloride compound containing 1/2 of water and a pharmaceutical composition preparation thereof. Each mole of cefmenoxime hydrochloride contains 1/2 mole of water. 7-amino-cephalosporanic acid (7ACA) is taken as a starting material, firstly reacts with 5-sulfydryl-1-methyl-1H-tetrazole (MMT) to generate 3-(1-methyl-1-tetrazole-5H) methyl sulfide-7-amino-cephalosporanic acid (7ACT) at C-3 position, then reacts with MAEM to synthesize cefmenoxime at C-7 position, and then reacts with hydrochloric acid to form salt, so that the cefmenoxime hydrochloride compound containing 1/2 of water is obtained. The operation is simple, the reactants are obtained easily, the reaction conditions are mild, and the yield is high. The cefmenoxime hydrochloride compoundcontaining 1/2 of water has low hygroscopicity, low impurity content, good mobility, good thermodynamic stability and wider application prospects.